The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-(Piperazin-1-yl)phenol( cas:56621-48-8 ) is researched.Recommanded Product: 56621-48-8.Kulig, Katarzyna; Sapa, Jacek; Maciag, Dorota; Filipek, Barbara; Malawska, Barbara published the article 《Synthesis and pharmacological evaluation of new 1-[3-(4-arylpiperazin-1-yl)-2-hydroxypropyl]-pyrrolidin-2-one derivatives with anti-arrhythmic, hypotensive, and α-adrenolytic activity》 about this compound( cas:56621-48-8 ) in Archiv der Pharmazie (Weinheim, Germany). Keywords: piperazine pyrrolidinone preparation antiarrhythmic hypotensive adrenolytic SAR. Let’s learn more about this compound (cas:56621-48-8).
A series of novel arylpiperazines bearing a pyrrolidin-2-one fragment was synthesized and evaluated for the binding affinity of the α1- and α2-adrenoceptors (AR) and for the antiarrhythmic and hypotensive activities of the compounds The most potent and selective compound 1-[2-hydroxy-3-[4-[(2-hydroxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one 8 binds with pKi = 6.71 for α1-AR. Derivative 8 (I) was also the most active in the prophylactic antiarrhythmic test in adrenaline-induced arrhythmia in anesthetized rats. Its ED50 value equals 1.9 mg/kg (i.v.). Compounds with substituents such as a fluorine atom 4, a Me 5, or a hydroxyl 8 group, or two substituents such as fluorine/chlorine atoms and methoxy groups in the Ph ring, significantly decreased the systolic and diastolic pressure in normotensive anesthetized rats at a dosages of 5-10 mg/kg (i.v.). It was found that the presence of the piperazine ring and a hydroxy group in the second position of the Pr chain are critical structural features in determining the affinity of the compounds tested.
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